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| | (7S)-6-(Cyclopropylmethyl)-2-(2,4-dichlorophenyl)-7-ethyl-7,8-dihydro-4-methyl-6H-1,3,6,8a-tetraazaacenaphthylene hydrochloride Basic information |
| Product Name: | (7S)-6-(Cyclopropylmethyl)-2-(2,4-dichlorophenyl)-7-ethyl-7,8-dihydro-4-methyl-6H-1,3,6,8a-tetraazaacenaphthylene hydrochloride | | Synonyms: | (7S)-6-(Cyclopropylmethyl)-2-(2,4-dichlorophenyl)-7-ethyl-7,8-dihydro-4-methyl-6H-1,3,6,8a-tetraazaacenaphthylene hydrochloride | | CAS: | 1782228-59-4 | | MF: | C21H23Cl3N4 | | MW: | 437.79 | | EINECS: | | | Product Categories: | | | Mol File: | 1782228-59-4.mol |  |
| | (7S)-6-(Cyclopropylmethyl)-2-(2,4-dichlorophenyl)-7-ethyl-7,8-dihydro-4-methyl-6H-1,3,6,8a-tetraazaacenaphthylene hydrochloride Chemical Properties |
| solubility | Soluble to 100 mM in water and to 100 mM in DMSO |
| | (7S)-6-(Cyclopropylmethyl)-2-(2,4-dichlorophenyl)-7-ethyl-7,8-dihydro-4-methyl-6H-1,3,6,8a-tetraazaacenaphthylene hydrochloride Usage And Synthesis |
| Uses | NBI 35965 Hydrochloride is a potent and selective corticotropin-releasing factor 1 (CRF1) antagonist. | | in vivo | NBI 35965 hydrochloride (20 mg/kg; oral gavage; once) reduces stress induced ACTH production in mice[1].
In rats, NBI 35965 hydrochloride (Compound 12a; 10 mg/kg) has a volume of distribution 17.8 L/kg, a plasma clearance of 17 mL/min/kg, and a half-life of 12 h. The estimated oral bioavailability is 34% with a mean maximal plasma concentration at 1 h of 560 ng/mL. NBI 35965 hydrochloride also penetrated the blood-brain barrier, resulting in a mean maximal brain concentration of 700 ng/g[1]. | Animal Model: | Male CD-1 mice (24-26 g) bearing restraint stress[1] | | Dosage: | 20 mg/kg (10 mL/kg 5% mannitol-d (w/v) in water) | | Administration: | Oral gavage; 60 min prior to the initiation of the stressor | | Result: | Reduced stress induced ACTH production in vivo.
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| | IC 50 | CRFR1: 4 nM (Ki); CRFR1: 8.5 (pKi) | | storage | Desiccate at RT |
| | (7S)-6-(Cyclopropylmethyl)-2-(2,4-dichlorophenyl)-7-ethyl-7,8-dihydro-4-methyl-6H-1,3,6,8a-tetraazaacenaphthylene hydrochloride Preparation Products And Raw materials |
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